sPLA₂-IIA Inhibitor II, KH064

A reversible, potent, and selective sPLA₂-IIA/PLA2g2a (phospholipase A2 group IIA) inhibitor (IC₅₀ = 29 nM) that displays much reduced potency against sPLA₂-V/PLA2g5 (PLA₂ group V; IC₅₀ = 2 µM) and is reported not to affect the activity of cytosolic cPLA₂, Ca²⁺-independent iPLA₂, 30 human GPCRs, and 25 other enzymes. In addition to being useful in studying PLA2g2a-mediated cellular responses in cultures in vitro (100% inhibition of LPS-induced PGE₂ production in HMC-1 cells; 15 min 10 µM pretreatment), KH064 is orally available in rats and efficacious in various rat disease models in vivo (5 mg/kg p.o.), including adjuvant-induced arthritis, spontaneous hypertension, high fat diet-induced metabolic disorders. Comparing to the substrate-competitive inhibitor c(2NapA)LS(2NapA)R (Cat. No. 525145), KH064 also effectively chelates sPLA₂-IIA active site Ca²⁺ in addition to targeting the enzyme′s N-terminal lipid substrate binding site.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Hansford, K. A., et al. 2003. Chembiochem.4, 181.
Iyer, A., et al. 2012. Diabetes.61, 2320,
Levick, S., et al. 2006. J Immunol.176, 7000.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)